3,N-Dihydroxy-propionamidine → {3-[3-(2-Hydroxyethyl)-1,2,4-oxadiazol-5-yl]-5-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}-(thiomorpholin-4-yl)methanone

HRID 220028Notes

Reaction equation

HRID 220028 reaction equation
[N:1]1([C:7]([N:9]2[CH2:14][CH:13]([C:15]3[CH:20]=[CH:19][C:18]([O:21][C:22]([F:25])([F:24])[F:23])=[CH:17][CH:16]=3)[CH2:12][CH:11]([C:26]([OH:28])=O)[CH2:10]2)=[O:8])[CH2:6][CH2:5][S:4][CH2:3][CH2:2]1.O[N:30]=[C:31]([NH2:35])[CH2:32][CH2:33][OH:34]>>[OH:34][CH2:33][CH2:32][C:31]1[N:35]=[C:26]([CH:11]2[CH2:12][CH:13]([C:15]3[CH:16]=[CH:17][C:18]([O:21][C:22]([F:23])([F:24])[F:25])=[CH:19][CH:20]=3)[CH2:14][N:9]([C:7]([N:1]3[CH2:6][CH2:5][S:4][CH2:3][CH2:2]3)=[O:8])[CH2:10]2)[O:28][N:30]=1

Participants

3

Reactant 2

HCID 34743873,N-Dihydroxy-propionamidineHCID 581165811-(Thiomorpholin-4-ylcarbonyl)-5-[4-(trifluoromethoxy)phenyl]piperidine-3-carboxylic acid

Product 1

HCID 59606582{3-[3-(2-Hydroxyethyl)-1,2,4-oxadiazol-5-yl]-5-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}-(thiomorpholin-4-yl)methanone

Procedure

According to General Method 6A, 1.00 g (2.390 mmol) of the compound from Example 25A and 323 mg (3.107 mmol) of N′,3-dihydroxypropanimidamide were reacted Yield: 848 mg (69% of theory)

Workup

  1. customwere reacted Yield: 848 mg (69% of theory)

Sources & evidence

ORD record
ord-99711d23873c4e12853ed0b84a84f926
Source dataset
uspto-grants-2012_06
Patent number
US08202862B2

Reaction notes

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